1442657-12-6

1442657-12-6 structure
1442657-12-6 structure
  • Name: Pasotuxizumab
  • Chemical Name: Pasotuxizumab
  • CAS Number: 1442657-12-6
  • Molecular Formula:
  • Molecular Weight:
  • Catalog: Research Areas Cancer
  • Create Date: 2023-04-25 16:57:22
  • Modify Date: 2024-01-04 13:32:20
  • Pasotuxizumab (BAY 2010112) is a PSMA and CD3 bispecific T-cell engager (BiTE). Pasotuxizumab binds to CD3 and PSMA with KDs of 9.4 nM and 47.0 nM for human CD3 and PSMA. Pasotuxizumab can be used for research of metastatic castration-resistant prostate cancer (mCRPC)[1][2].

Name Pasotuxizumab
Description Pasotuxizumab (BAY 2010112) is a PSMA and CD3 bispecific T-cell engager (BiTE). Pasotuxizumab binds to CD3 and PSMA with KDs of 9.4 nM and 47.0 nM for human CD3 and PSMA. Pasotuxizumab can be used for research of metastatic castration-resistant prostate cancer (mCRPC)[1][2].
Related Catalog
Target

KDs: 9.4 nM and 16.3 nM for human and cynomolgus monkey CD3. KDs: 47.0 nM and 212.6 nM for human and cynomolgus monkey PSMA.

In Vitro Pasotuxizumab (约 0-100 ng/mL,48 小时) 可激活 CD4+ 和 CD8+ T 细胞群,EC50 为 3.4-6.7 ng/mL (人) 和 13.7-21.2 ng/mL (食蟹猴)[2]。 Pasotuxizumab (约 0-100 ng/mL,48 小时) 增加 T 细胞中干扰素-γ、TNF-α、IL-2 和 IL-10 的释放[2]。
In Vivo Rafivirumab (0.005-5 mg/kg,尾静脉注射,每日一次) 抑制 PC-3-huPSMA 小鼠异种移植模型中的肿瘤生长[2]。 Rafivirumab (0.1-1 mg/kg,静脉推注给药) 在 BALB/c 小鼠中表现出较低的血清清除率[2]。 Animal Model: PC-3-huPSMA mouse xenograft model[2] Dosage: 0.005-5 mg/kg Administration: i.v., once daily Result: Inhibited tumor growth by 86% (0.005 mg/kg/d) and 99% (5 mg/kg/d). Animal Model: BALB/c mice (PK Assay)[2] Dosage: 0.1, 0.3, and 1 mg/kg Administration: i.v. bolus administration or s.c. Result: Pharmacokinetic profile of Rafivirumab. Dose (mg/kg) AUC (mg h/L) CLmatrix (L/h/kg) T1/2 (h) F (%) i.v. (0.3) 0.93 0.32 9.7 100 s.c. (0.3) 0.17 11 18
References

[1]. Horst-Dieter Hummel, et al. Phase 1 study of pasotuxizumab (BAY 2010112), a PSMA-targeting Bispecific T cell Engager (BiTE) immunotherapy for metastatic castration-resistant prostate cancer (mCRPC). Journal of Clinical Oncology 2019 37:15_suppl, 5034-5034.

[2]. Friedrich M, et al. Regression of human prostate cancer xenografts in mice by AMG 212/BAY2010112, a novel PSMA/CD3-Bispecific BiTE antibody cross-reactive with non-human primate antigens. Mol Cancer Ther. 2012 Dec;11(12):2664-73.  

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